Bisoprolol-SZ, pills 10mg, 50pcs

Composition

Active ingredient:  

bisoprolol fumarate 5 mg and 10 mg

Auxiliary substances:

kernel – croscarmellose sodium (I primel – vine) – 2.2 mg,4.4 mg;

povidone (polyvinylpyrrolidone middle) – 6.0 mg,12.0 mg;

pregelatinization starch (starch 1500) – 4.0 mg,8.0 mg;

silicon dioxide colloidal (Aerosil) – 1,54 mg,3.08 mg;

talc – 2.0 mg,4.0 mg;

cellulose microcrystalline – 30,4 mg of 60.8 mg;

lactose (milk sugar) – 47,86 mg,95,72 mg;

magnesium stearate – 1.0 mg;

shell – Opadry II (polyvinyl alcohol, partially hydrolyzed – 1.2 mg,2.4 mg; titanium dioxide – 0,67998 mg,1,35996 mg; talc – 0,444 mg,0,888 mg; macrogol (polyethylene glycol 3350) – 0,606 mg,1,212 mg; dye iron oxide (II) yellow – 0,07002 mg,0,14004 mg).

Pharmacological action

Selective betagadren blocker, without its own sympathomimetic activity, does not have a membrane-stabilizing effect. Reduces the activity of blood plasma renin, reduces the need for myocardial oxygen, reduces the heart rate (HR) (at rest and during exercise).

It has antihypertensive, antiarrhythmic and anti-anginal effects. By blocking the betagadrenoreceptors of the heart in low doses, it reduces the catecholamine – stimulated formation of cAMP from ATP, reduces the intracellular flow of calcium ions, has a negative chrono -, dromo -, batmo-and inotropic effect, inhibits conduction and excitability, and reduces atrioventricular conduction.

When the dose is increased above the therapeutic level, it has a beta-2-adrenoblocking effect.

Total peripheral vascular resistance at the beginning of the drug use, in the first 24 hours, increases (as a result of a reciprocal increase in alpha-adrenergic activity and elimination of beta-2-adrenergic stimulation), which returns to the initial value after 1-3 days, and decreases with prolonged use.

The hypotensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (which is of great importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure (BP), and an effect on the central nervous system (CNS).

With arterial hypertension, the effect occurs in 2-5 days, stable effect – in 1-2 months. The antianginal effect is due to a decrease in the myocardial oxygen demand as a result of a decrease in heart rate and contractility, an elongation of the diastole, and an improvement in myocardial perfusion.

By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, it can increase the need for oxygen, especially in patients with chronic heart failure.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers, and a slowdown in atrioventricular (AV) conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the AV node) and along additional pathways.

When used in medium therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing beta-2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause a delay in sodium (Na+) ions in the body; the severity of the atherogenic effect does not differ from that of propranolol.

Pharmacokinetics

Absorption – 80-90%, food intake does not affect the absorption. The maximum concentration in the blood plasma is observed after 1-3 hours, the connection with plasma proteins is about 30%. Permeability through the blood-brain barrier and placental barrier is low, and secretion with breast milk is low.

50% of the dose is metabolized in the liver to form inactive metabolites, with a half-life of 10-12 hours. About 98% is excreted by the kidneys – 50% unchanged, less than 2% with bile.

Indications

• Arterial hypertension;

• ischemic heart disease: prevention of angina attacks.

Use during pregnancy and lactation

Use during pregnancy and lactation is possible if the benefit to the mother exceeds the risk of side effects in the fetus and child.

Contraindications

Hypersensitivity to the components of the drug and other beta – blockers, shock (including cardiogenic), collapse, pulmonary edema, acute heart failure, chronic heart failure in the decompensation stage, atrioventricular (AV) block II-III art., sinoatrial block, sinus node weakness syndrome, severe bradycardia, Prinzmetal angina pectoris, cardiomegaly (without signs of heart failure), arterial hypotension (systolic blood pressure less than 100 mm Hg, especially in cases of myocardial infarction); severe forms of bronchial asthma and a history of chronic obstructive pulmonary disease; concomitant use of monoamine oxidase (MAO)inhibitors (with the exception of MAO-B), late-stage peripheral circulatory disorders, Raynaud’s disease), pheochromocytoma (without simultaneous use of alpha-blockers), metabolic acidosis, age up to 18 years (efficacy and safety have not been established).

With caution: liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, diabetes mellitus, atrioventricular block I degree, depression (including in the anamnesis), psoriasis, elderly age.

Side effects

From the central nervous system: increased fatigue, weakness, dizziness, headache, sleep disorders, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenia, myasthenia gravis, paresthesia in the extremities (in patients with “intermittent” claudication and Raynaud’s syndrome), tremor.

From the sensory organs: visual impairment, decreased secretion of lacrimal fluid, dry and painful eyes, conjunctivitis.

From the cardiovascular system: sinus bradycardia, palpitation, impaired myocardial conduction, AV block (up to the development of complete transverse block and cardiac arrest), arrhythmias, weakening of myocardial contractility, development (aggravation) of chronic heart failure (swelling of the ankles, feet, shortness of breath), decrease in blood pressure, orthostatic hypotension, angiospasm manifestation (increased peripheral circulatory disorders, cold of the lower extremities, syndrome Raynaud’s disease), chest pain.

From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, liver function disorders (dark urine, jaundice of the sclera or skin, cholestasis), taste changes.

From the respiratory system: nasal congestion, difficulty breathing when prescribed in high doses (loss of selectivity) and/or in predisposed patients – laryngo – and bronchospasm.

From the endocrine system: hyperglycemia (in patients with insulin – dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroidism.

Allergic reactions: pruritus, rash, urticaria.

From the skin: increased sweating, hyperemia of the skin, exanthema, psoriasis-like skin reactions, exacerbation of psoriasis symptoms.

Laboratory parameters: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, changes in the activity of liver enzymes (increased ALT, ACT), bilirubin levels, triglycerides. Effects on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

Others: back pain, arthralgia, decreased libido, decreased potency, withdrawal syndrome (increased angina attacks, increased blood pressure).

Interaction

Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol.

Iodine-containing radiopaque drugs for intravenous use increase the risk of developing anaphylactic reactions. Phenytoin with intravenous use, drugs for inhaled general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive effects and the likelihood of lowering blood pressure. Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure). Reduces the clearance of lidocaine and xanthines (except diphylline) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking.

The antihypertensive effect is weakened by nonsteroidal anti-inflammatory drugs (Na+ delay and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids and estrogens (Na+ion delay).

Cardiac glycosides, methyldopa, reserpine and guanfacine, slow calcium channel blockers (verapamil, diltiazem), amiodorone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV block, cardiac arrest and heart failure. Nifedipine can lead to a significant decrease in blood pressure.

Diuretics, clonidine, sympatholytics, hydralazine, and other antihypertensive medications can lead to an excessive decrease in blood pressure. It prolongs the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.

Tri-and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives, and sleeping pills increase CNS depression.

Concomitant use with MAO inhibitors is not recommended due to a significant increase in the antihypertensive effect, a break in treatment between taking MAO inhibitors and bisoprolol should be at least 14 days.

Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.

Ergotamine increases the risk of developing peripheral circulatory disorders; sulfasalazine increases the concentration of bisoprolol in plasma; rifampicin shortens the half-life.

How to take, course of use and dosage

Inside, in the morning on an empty stomach, without chewing,5 mg once. If necessary, the dose is increased to 10 mg once a day. The maximum daily dose is 20 mg / day.

In patients with impaired renal function with creatine clearance less than 20 ml/min or with severe hepatic impairment, the maximum daily dose is 10 mg. No dose adjustment is required in elderly patients.

Overdose

Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV block, marked decrease in blood pressure, chronic heart failure, cyanosis of the fingernails or palms, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.

Treatment: gastric lavage and use of adsorbents; symptomatic therapy: if AV block develops – intravenous use of 1-2 mg of atropine, epinephrine or a temporary pacemaker; with ventricular extrasystole – lidocaine (class IA drugs are not used ); with a decrease in blood pressure – the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema – intravenous plasma – substituting solutions, if ineffective – use of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic effects and eliminate a pronounced decrease in blood pressure); in heart failure – cardiac glycosides, diuretics, glucagon; in convulsions-IV diazepam; in bronchospasm, beta-adrenostimulants by inhalation.

Special instructions

Use with caution for psoriasis and indications of psoriasis in the family history, diabetes mellitus in the decompensation phase, with a predisposition to allergic reactions. With pheochromocytoma, the use of bisoprolol is possible only after taking alpha-blockers. To avoid sudden withdrawal of bisoprolol, the course of treatment should be completed slowly with a gradual decrease in the dose.

Storage conditions

Store in a dry place protected from light, out of reach of children, at a temperature not exceeding 20 °C.

Shelf

life is 3 years.

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Arrhythmia, Hypertension, Heart Failure